Product Name: CNX-1351
CNX-1351 Chemical Structure
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CNX-1351 is an orally active selective inhibitor of PKB/Akt, a key enzyme in the PI3K/PKB/mTOR tumour cell survival pathway, and dysregulation of this pathway leads to tumour resistance to a number of important anti-cancer drugs.
CNX-1351 is a selective covalent Inhibitor of PI3Kα. CNX-1351 was tested against all four of the class I PI3K enzymes α, β, γ, and δ. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α.
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